Letters in Drug Design & Discovery

Editor-in-Chief

K. Kuca
University of Hradec Kralove
Hradec Kralove
(Czech Republic)

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Open Access Articles

Structure-based Drug Design Strategies in the Development of Small Molecule Inhibitors Targeting Bcl-2 Family Proteins open Access plus

Volume: 17   Issue: 8
Pp: 943-953
Zhe Yin, Donglin Yang, Jun Wang and Yuequan Jiang*
DOI:10.2174/1570180817666200213114759

Comparison in the Glucose Response of Flexible Liposomes Loaded with Insulin with the Addition of Different Surfactants in an Experimental Diabetes Model open Access plus

Volume: 17   Issue: 6
Pp: 787-798
Sara Melisa Arciniegas , Sergio Andres Saavedra , Danaé Balderas , Sara del Carmen Caballero, María Josefa Bernad, Julio Cesar Sánchez , María Isabel Gracia, Héctor Ariel Rico and Dinorah Vargas *
DOI:10.2174/1570180816666191024102231

Identification of Phosphoinositide-3 Kinases Delta and Gamma Dual Inhibitors Based on the p110δ/γ Crystal Structure open Access plus

Volume: 17   Issue: 6
Pp: 772-786
Wen-Qing Jia , Xiao-Yan Feng, Ya-Ya Liu , Zhen-Zhen Han , Zhi Jing, Wei-Ren Xu and Xian-Chao Cheng*
DOI:10.2174/1570180816666190730163431

Synthesis, Characterization, and Molecular Docking Studies of N-Acylated Butyro and Valerolactam Derivatives with Antiproliferative and Cytotoxic Activities open Access plus

Volume: 17   Issue: 6
Pp: 725-730
Mark Tristan J. Quimque, Mark John P. Mandigma, Justin Allen K. Lim, Simon Budde, Hans-Martin Dahse, Oliver B. Villaflores, Arnold V. Hallare and Allan Patrick G. Macabeo*
DOI:10.2174/1570180816666190716141524

Synthesis and Evaluation of Anticonvulsant Activities of 4-Phenylpiperidin- 2-one Derivatives open Access plus

Volume: 17   Issue: 6
Pp: 713-724
Shi-Ben Wang*, Hui Liu, Guang-Yong Li, Kang Lei, Xiao-Jing Li, Zhe-Shan Quan and Xue-Kun Wang*
DOI:10.2174/1570180816666190710142848

Mannitol Reduces Spinal Cord Edema in Rats with Acute Traumatic Spinal Cord Injury open Access plus

Volume: 17   Issue: 6
Pp: 676-683
Chao Zhang, Anming Hu, Yingli Jing, Degang Yang* and Jianjun Li*
DOI:10.2174/1570180816666190731112158

Azacyanines as Novel Topoisomerase II Alpha Inhibitors open Access plus

Volume: 17   Issue: 5
Pp: 666-671
Sercan Guloglu, Fahriye Nur Kirmaci, Özgül Persil Çetinkol*, Mehrdad Forough and Aybuke Gulkaya
DOI:10.2174/1570180816666190628161945

Microwave-assisted Synthesis and Docking Studies of Phenylureas as Candidates for the Drug Design Against the Biological Warfare Agent Yersinia Pestis open Access plus

Volume: 17   Issue: 5
Pp: 633-639
Tanos Celmar Costa França*, Leonardo da Costa Bastos, Teobaldo Cuya, Mehdi Sirouspour, Franklin Chacón-Huete, David Bendahan and Pat Forgione*
DOI:10.2174/1570180816666190710144212

Design of New Therapeutic Agents Targeting FLT3 Receptor Tyrosine Kinase Using Molecular Docking and 3D-QSAR Approach open Access plus

Volume: 17   Issue: 5
Pp: 585-596
Swapnil Pandurang Bhujbal, Seketoulie Keretsu and Seung Joo Cho*
DOI:10.2174/1570180816666190618104632

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone open Access plus

Volume: 17   Issue: 4
Pp: 512-517
Ognyan Ivanov Petrov, Yordanka Borisova Ivanova*, Mariana Stefanova Gerova and Georgi Tsvetanov Momekov
DOI:10.2174/1570180816666190730164952

New Hydrazone Derivatives of Pyrazole-4-carboxaldehydes Exhibited Anti-inflammatory Properties open Access plus

Volume: 17   Issue: 4
Pp: 502-511
Mingxia Song, Bing Liu, Shengwang Yu, Shihui He, Yuqiu Liang, Sifan Li, Qiuyan Chen and Xianqing Deng*
DOI:10.2174/1570180816666190731113441

In Silico Elucidation of the Molecular Recognition of Phenol Derivative Compounds and Hippuryl-histidyl-leucine as an Artificial Substrate with the Experimental Target: Angiotensin-converting Enzyme open Access plus

Volume: 17   Issue: 4
Pp: 445-466
Víctor Hugo Vázquez-Valaldez*, Manuel Alejandro Hernández S, Ivonne Carrillo Cedillo, Ana María Velázquez Sanchez, Mildred Sauce Guevara, Rafael López Castañares and Enrique Ángeles
DOI:10.2174/1570180816666190906155034

In vitro and In Vivo Evaluation of Quinoxaline 1,4-di-N-oxide Against Giardia lamblia open Access plus

Volume: 17   Issue: 4
Pp: 428-433
Elizabeth Barbosa-Cabrera, Rosa Moo-Puc, Antonio Monge, Alma Delia Paz-González, Virgilio Bocanegra-García and Gildardo Rivera*
DOI:10.2174/1570180816666190618115854

Carbon Nanotubes Enhance the Chemotherapy Sensitivity of Tumors with Multidrug Resistance open Access plus

Volume: 17   Issue: 4
Pp: 366-378
Zhijie Wang, Jinhua Tao, Jianan Chen and Qian Liu*
DOI:10.2174/1570180816666190405110858

Drug Discovery of Acetophenone Derivatives as BRD4 Inhibitors open Access plus

Volume: 17   Issue: 3
Pp: 323-329
Zhimin Zhang, Wenhai Huang, Xiaoliang Zheng, Chuansheng Li and Zhengrong Shen*
DOI:10.2174/1570180816666190329223559

A Series of Furan-based Hydrazones: Design, Synthesis, and Evaluation of Antimicrobial Activity, Cytotoxicity and Genotoxicity open Access plus

Volume: 17   Issue: 3
Pp: 312-322
Mehlika Dilek Altintop*, Belgin Sever, Özlem Atli Eklioğlu, Merve Baysal, Rasime Demirel and Ahmet Özdemir
DOI:10.2174/1570180816666190325163948

Novel Strobilurin Derivatives Containing Carboxylate Unit as Potential Antifungal Agents open Access plus

Volume: 17   Issue: 3
Pp: 300-311
Longzhu Bao, Shuangshuang Wang, Di Song, Jingjing Wang, Xiali Yue and Xiufang Cao*
DOI:10.2174/1570180816666190325164452

Synthesis of Limonin Derivatives with Improved Anti-inflammatory and Analgesic Properties open Access plus

Volume: 17   Issue: 3
Pp: 285-299
Chengshu Jia, Bin Hu, Yingying Ji, Yourui Su, Guoqing Gong, Qihua Zhu and Yungen Xu*
DOI:10.2174/1570180816666181113102359

New Hybrids Derived from the Natural Compound (-)-β-Pinene and Amides or Acylthioureas as Antitumor Agents open Access plus

Volume: 17   Issue: 3
Pp: 271-284
Shengliang Liao, Xiaoping Rao, Minggui Shen, Hongyan Si, Jie Song, Shibin Shang* and Zhanqian Song*
DOI:10.2174/1570180816666181107094427

Synthesis of Piperidine Conjugated Dihydroquinazolin-4(1H)-ones and their Antiproliferative Activity, Molecular Docking Studies and DFT Calculations open Access plus

Volume: 17   Issue: 1
Pp: 85-93
Kereyagalahally Honneshappa Narasimhamurthy, Chandra, Toreshettahally Ramesh Swaroop, Swamy Jagadish and Kanchugarakoppal Subbegowda Rangappa*
DOI:10.2174/1570180816666190613120349

Synthesis and Analgesic Activity of Monoterpenoid Aldehyde-derived Hydro-2H-chromeneols open Access plus

Volume: 17   Issue: 1
Pp: 68-78
Irina Il'ina*, Ekaterina Morozova, Dina Korсhagina, Konstantin Volсho, Tat'yana Tolstikova and Nariman Salakhutdinov
DOI:10.2174/1570180816666181114131220

Identifying the Structural Features of Diphenyl Ether Analogues for InhA Inhibition: A 2D and 3D QSAR Based Study open Access plus

Volume: 17   Issue: 1
Pp: 31-47
Ashutosh Prasad Tiwari, Varadaraj Bhat Giliyar*, Gurypur Gautham Shenoy and Vandana Kalwaja Eshwara
DOI:10.2174/1570180816666190611153933

Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators open Access plus

Volume: 16   Issue: 12
Pp: 1387-1394
Mark Gallant Fulton, Matthew Thomas Loch, Caroline Anne Cuoco, Alice Lambert Rodriguez, Emily Days, Paige Newton Vinson, Krystian Andrezej Kozek, Charles David Weaver, Anna Louise Blobaum, Peter Jeffrey Conn, Colleen Marie Niswender* and Craig William Lindsley*
DOI:10.2174/1570180815666181017131349

Antitumor Activity of Cyclodextrin-based Supramolecular Platinum Prodrug In vitro and In vivo open Access plus

Volume: 16   Issue: 11
Pp: 1296-1301
Yu-Hui Zhang, Jie Wang, Siqintana Xin, Li-Juan Wang and Xianliang Sheng*
DOI:10.2174/1570180816666190618114505

Synthesis of Phenyl- and Pyridyl-substituted Benzyloxybenzaldehydes by Suzuki-Miyaura Coupling Reactions open Access plus

Volume: 16   Issue: 11
Pp: 1248-1257
Hedvig Bölcskei*, Andrea Német-Hanzelik, Zsófia Dubrovay, Viktor Háda and György Keglevich
DOI:10.2174/1570180816666181106123809

Effects of Dietary Intake and Supplementation of Fatty Acids on Cardiometabolic Disorders in Humans: a Lesson from a Large Number of Meta-Analyses open Access plus

Volume: 16   Issue: 10
Pp: 1138-1145
Sho-ichi Yamagishi* and Takanori Matsui
DOI:10.2174/1570180816666181107113148

Benzo[d]imidazol-5-yl)-5-(substituted)-1,3,4-Oxadiazoles: Synthesis, Anticancer, Antimicrobial and In Silico Studies open Access plus

Volume: 16   Issue: 9
Pp: 994-1005
Naveen Kumar, Swamy Sreenivasa*, Bhuvanesh Sukhlal Kalal, Vasantha Kumar, Bantwal Shivarama Holla, Vinitha Ramanath Pai, Nadigar Revansiddappa Mohan and Shivaraj Govindaiah
DOI:10.2174/1570180816666181220123924

The Structure of MT189-Tubulin Complex Provides Insights into Drug Design open Access plus

Volume: 16   Issue: 9
Pp: 1069-1073
Zhongping Li, Lingling Ma, Chengyong Wu, Tao Meng, Lanping Ma, Wenyue Zheng, Yamei Yu*, Qiang Chen*, Jinliang Yang and Jingkang Shen
DOI:10.2174/1570180816666181122122655

Synthesis and Evaluation of in vitro Antiplatelet Aggregation Activities of 2-Methoxy-5-Aminobenzamides open Access plus

Volume: 16   Issue: 9
Pp: 1040-1050
Lili Liu, Xiujie Liu*, Guangling Chen and Kai Qiu
DOI:10.2174/1570180816666181128105044

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents open Access plus

Volume: 16   Issue: 9
Pp: 1020-1030
Zhaochang Liang, Yuping Huang, Shiben Wang and Xianqing Deng*
DOI:10.2174/1570180816666190325163117

In Vitro and In Vivo Profiles and Characterization of Insulin Nanocarriers Based in Flexible Liposomes Designed for Oral Administration open Access plus

Volume: 16   Issue: 8
Pp: 948-960
Sara Melisa Arciniegas Ruiz, María Josefa Bernad Bernad, Raquel Lopez Arellano, Roberto Diaz Torres, Sara Del Carmen Caballero Chacón and Dinorah Vargas Estrada*
DOI:10.2174/1570180816666190110112929

Synthesis, Anti-inflammatory, Antimicrobial Potential and Molecular Docking Studies of 4,5-Disubstituted-1,2,4-Triazole Thioacetate Derivatives open Access plus

Volume: 16   Issue: 7
Pp: 734-745
Muhammad Nouman Arif, Humaira Nadeem*, Rehan Zafar Paracha, Arif-ullah Khan, Muhammad Imran and Fawad Ali
DOI:10.2174/1570180815666180810122226

Design and Synthesis of the Diazirine-based Clickable Photo-affinity Probe Targeting Sphingomyelin Synthase 2 open Access plus

Volume: 16   Issue: 6
Pp: 678-684
Penghui Wang, Zhining Li, Lulu Jiang, Lu Zhou* and Deyong Ye*
DOI:10.2174/1570180816666181106154601

Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents open Access plus

Volume: 16   Issue: 4
Pp: 446-452
Mashooq Ahmad Bhat*, M. Al-Tahhan, Mohamed A. Al-Omar, Ahmed M. Naglah and Abdullah Al-Dhfyan
DOI:10.2174/1570180815666181008100944

A Study on the Synthesis of Risedronic Acid: The Role of an Ionic Liquid Additive open Access plus

Volume: 16   Issue: 3
Pp: 238-244
Dávid Illés Nagy, Alajos Grün, Júlia Sinkovicz, Sándor Garadnay, István Greiner and György Keglevich*
DOI:10.2174/1570180815666180626122630

Synthesis and Biological Evaluation of Some Novel Thiophene-bearing Quinazoline Derivatives as EGFR Inhibitors open Access plus

Volume: 16   Issue: 2
Pp: 102-110
Min Zou, Bo Jin, Yanrong Liu, Huiping Chen, Zhuangli Zhang, Changzheng Zhang, Zhihong Zhao and Liyun Zheng*
DOI:10.2174/1570180815666180803125935

Efficient Synthesis of Ibandronate in the Presence of an Ionic Liquid open Access plus

Volume: 15   Issue: 7
Pp: 713-720
David Illes Nagy, Alajos Grun, Oliver Pavela, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich*
DOI:10.2174/1570180814666171027160324

L-carnitine Supplementation Improves Self-rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis open Access plus

Volume: 14   Issue: 6
Pp: 737-742
Kyoko Tashiro, Yusuke Kaida, Sho-ichi Yamagishi, Hideharu Tanaka, Miyuki Yokoro, Junko Yano, Kazuko Sakai, Yuka Kurokawa, Kensei Taguchi, Yosuke Nakayama, Takahiro Inokuchi and Kei Fukami*
DOI:10.2174/1570180814666170216102632

The Synthesis of (Iodobenzyl)oxybenzaldehydes, Useful Intermediates for Biologically Active Targets open Access plus

Volume: 14   Issue: 2
Pp: 233-239
Hedvig Bölcskei, Andrea Német-Hanzelik, István Greiner, Zsófia Dubrovay, Viktor Háda and György Keglevich
DOI:10.2174/1570180813666160804142245

In Vitro and In Vivo Investigations into the Carbene Gold Chloride and Thioglucoside Anticancer Drug Candidates NHC-AuCl and NHC-AuSR open Access plus

Volume: 14   Issue: 2
Pp: 125-134
Wolfgang Walther, Oyinlola Dada, Cillian O’Beirne, Ingo Ott, Goar Sánchez-Sanz, Claudia Schmidt, Carsta Werner, Xiangming Zhu and Matthias Tacke
DOI:10.2174/1570180813666160826100158

Efficient Synthesis of Pamidronic Acid Using an Ionic Liquid Additive open Access plus

Volume: 13   Issue: 6
Pp: 475-478
Alajos Grun, Dávid Illés Nagy, Sándor Garadnay, István Greiner and Gyorgy Keglevich
DOI:10.2174/1570180812666151022221805

Potent and Orally Bioavailable Antiplatelet Agent, PLD-301, with the Potential of Overcoming Clopidogrel Resistance open Access plus

Volume: 13   Issue: 3
Pp: 250-254
Jingyu Chen and Michael Zhiyan Wang
DOI:10.2174/1570180812666150730221941

The Synthesis of Risedronic Acid and Alendronate Applying Phosphorus Oxychloride and Phosphorous Acid in Methanesulfonic Acid open Access plus

Volume: 12   Issue: 4
Pp: 253-258
Alajos Grun, Rita Kovacs, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich
DOI:10.2174/1570180811666141010220427

4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls open Access plus

Volume: 12   Issue: 2
Pp: 131-139
Maria Antonietta Dettori, Davide Fabbri, Marina Pisano, Carla Rozzo, Giuseppe Palmieri, Alessandro Dessi, Roberto Dallocchio and Giovanna Delogu
DOI:10.2174/1570180811666140915222343

Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking open Access plus

Volume: 11   Issue: 3
Pp: 331-338
Muhammad Yar, Marek Bajda, Rana Atif Mehmood, Lala Rukh Sidra, Nisar Ullah, Lubna Shahzadi, Muhammad Ashraf, Tayaba Ismail, Sohail Anjum Shahzad, Zulfiqar Ali Khan, Syed Ali Raza Naqvi and Nasir Mahmood
DOI:10.2174/15701808113106660078

Optimized Synthesis of Etidronate open Access plus

Volume: 10   Issue: 8
Pp: 733-737
Rita Kovacs, David Illes Nagy, Alajos Grün, Gyorgy Tibor Balogh, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich
DOI:10.2174/15701808113109990026

Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) open Access plus

Volume: 8   Issue: 5
Pp: 406-421
Kuiying Xu, Marie Wetzel, Rolf W. Hartmann and Sandrine Marchais-Oberwinkler
DOI:10.2174/157018011795514230

Phenylpyazoleanilides as Potent Inhibitor of IL-15 Dependent T Cell Proliferation. Part 2: Discovery of a New Drug Candidate, Y-320 open Access plus

Volume: 5   Issue: 4
Pp: 292-296
Hiroyuki Ushio, Seigo Ishibuchi, Kunitomo Adachi, Kouichi Oshita and Kenji Chiba
DOI:10.2174/157018008784619861

Selective Androgen Receptor Modulators Antagonize Apolipoprotein E4-Induced Cognitive Impairments open Access plus

Volume: 5   Issue: 4
Pp: 271-276
Summer Acevedo, Luis Gardell, Stefania Risso Bradley, Fabrice Piu and Jacob Raber
DOI:10.2174/157018008784619898

Phenylpyazoleanilides as a Potent Inhibitor of IL-15 Dependent T Cell Proliferation. Part 1: A New Class of Orally Available Immunomodulators open Access plus

Volume: 5   Issue: 2
Pp: 111-115
Hiroyuki Ushio, Seigo Ishibuchi, Kunitomo Adachi, Kouichi Oshita and Kenji Chiba
DOI:10.2174/157018008783928427