Background: A wide range of heterocyclic steroidal derivatives gained a special attention due to their
wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs
containing the steroid nucleus are known in the market.
Objective: Our main aim of this work was to synthesise a series of heterocyclic compounds especially thiophene
and thienopyridine derivatives containing the estrone nucleus. The synthesized compounds posses antitumor and
Method: Thiophene derivatives of estrone were synthesized and used for further heterocyclization reactions
through the reaction with the different reagent.
Results: Antiproliferative evaluations and c-Met kinase, Pim-1 kinase inhibitions were performed where some
compounds revealed high activities.
Conclusion: Compounds that showed high antiproliferative activity and c-Met- kinase inhibitions were tested
for all compounds. The most promising compounds 3b, 5c, 6c, 8d, 8f, 13e, 13f, 18b and 20d were further investigated
against tyrosine kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 6b, 13b, 16b and 16c
were selected to examine their Pim-1 kinase inhibition activity where compounds 11c, 18b and 20f showed high
activities. Structure-Activity Relationship (SAR) was rationalized by looking at the varying structural features of