Journal of Chemical and Pharmaceutical Research (ISSN : 0975-7384)

Reach Us reach to JOCPR whatsapp-JOCPR +44 1625708989
All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.

Original Articles: 2017 Vol: 9 Issue: 8

Design, Synthesis, Antitumor Activity, Cell Cycle Analysis and ELISA Assay for CDK-2 of a New (4-Aryl-6-Flouro-4H-Benzo [4, 5] Thieno [3, 2-b] Pyran) Derivatives


A series of benzo [1] thiophene derivatives (3a-f), (4a-f) and (5a-f) were synthesized and characterized by spectroscopic and elemental analysis. All compounds were subjected to one dose anticancer screening in NCI- America, but the only high results were further subjected to five dose screening. An outstanding result of compound 4f (GI50 = 0.15, TGI= 1.14 μM) and 4c (GI50 = 1.09, TGI = 10.19, LC50 = 100 μM). To explore mechanism of cytotoxicity, compound 4f and 4c were allowed to affect cell cycle using HT-29 cell line for (24 and 48 hr). They caused induction of apoptosis causing preG1 apoptosis and cell growth arrest at G2/M in a time dependant manner inhibiting CDK-2. IC50 of compound 5d was 0.32 μM, IC50 of 6 was 0.15 μM while IC50 of erlotinib reference was 0.3 μM. Finally we synthesized a series of benzo [1] thiophene derivatives having a good cytotoxic activity suggesting promising anticancer derivatives.

rtp slot demo