RRC ID 69288
Author Ramesh V, Ananda Rao B, Sharma P, Swarna B, Thummuri D, Srinivas K, Naidu VG, Jayathirtha Rao V.
Title Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
Journal Eur J Med Chem
Abstract Several rhodanine derivatives (9-39) were synthesized for evaluation of their potential as anticancer agents. Villsmeier cyclization to synthesize aza-aromatic aldehydes, rhodanine derivatives preparation and Knoevenagel type of condensation between the rhodanines and aza-aromatic aldehydes are key steps used for the synthesis of 31 compounds. In vitro antiproliferative activity of the synthesized rhodanine derivatives (9-39) was studied on a panel of six human tumor cell lines viz. HGC, MNK-74, MCF-7, MDAMB-231, DU-145 and PC-3 cell lines. Some of the compounds were capable of inhibiting the proliferation of cancer cell lines at a micromolar concentration. Six compounds are found to be potent against HGC cell lines; compound 15 is found to be active against HGC - Gastric, MCF7 - Breast Cancer and DU145 - Prostate Cancer cell lines; compound 39 is potent against MNK-74; four compounds are found to be potent against MCF-7 cell lines; three compounds are active against MDAMB-231; nine compounds are found to be potent against DU-145; three compounds are active against PC-3 cell lines. These compounds constitute a promising starting point for the development of novel and more potent anticancer agents in future.
Volume 83
Pages 569-80
Published 2014-8-18
DOI 10.1016/j.ejmech.2014.06.013
PII S0223-5234(14)00532-7
PMID 24996143
MeSH Antineoplastic Agents / chemical synthesis* Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Cell Line, Tumor Cell Proliferation / drug effects Drug Design* Humans Quinolines / chemistry* Rhodanine / chemical synthesis* Rhodanine / chemistry Rhodanine / pharmacology*
IF 5.573
Human and Animal Cells MKN74(RCB1002) DU145(RCB2143) PC-3(RCB2145)