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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Mini-Review Article

Structural Aspects of mTOR Inhibitors: Search for Potential Compounds

Author(s): Kamalpreet Kaur, Arjun Anant and Vivek Asati*

Volume 22, Issue 6, 2022

Published on: 20 July, 2021

Page: [1037 - 1055] Pages: 19

DOI: 10.2174/1871520621666210720121403

Price: $65


mTOR (mammalian target of rapamycin) is a catalytic subunit composed of two multi-protein complexes that indicate mTORC1 and mTORC2. It plays a crucial role in various fundamental cell processes like cell proliferation, metabolism, survival, cell growth, etc. Various first line mTOR inhibitors such as Rapamycin, Temsirolimus, Everolimus, Ridaforolimus, Umirolimus, and Zotarolimus have been used popularly. In contrast, several mTOR inhibitors such as Gedatolisib (PF-05212384) are under phase 2 clinical trials studies for the treatment of triple-negative breast cancer. The mTOR inhibitors bearing heterocyclic moieties such as quinazoline, thiophene, morpholine, imidazole, pyrazine, furan, quinoline are under investigation against various cancer cell lines (U87MG, PC-3, MCF-7, A549, MDA-231). In this review, we summarized updated research related to mTOR inhibitors and their structure-activity relationship, which may help scientists develop potent inhibitors against cancer.

Keywords: Anti-cancer, mTOR pathways, SAR, pyrimidine derivatives, heterocyclic compounds, triple-negative breast cancer.

Graphical Abstract
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