| RRC ID |
69288
|
| 著者 |
Ramesh V, Ananda Rao B, Sharma P, Swarna B, Thummuri D, Srinivas K, Naidu VG, Jayathirtha Rao V.
|
| タイトル |
Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
|
| ジャーナル |
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.
|
| 巻・号 |
83
|
| ページ |
569-80
|
| 公開日 |
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
|
| リソース情報 |
| ヒト・動物細胞 |
MKN74(RCB1002)
DU145(RCB2143)
PC-3(RCB2145) |
