Synthesis and anti-tumor evaluation of B-ring substituted steroidal pyrazoline derivatives.
The synthesis and anti-tumor activity screening of new steroidal derivatives (4-18) containing pharmacologically attractive pyrazoline moieties are performed. During in vitro anticancer evaluation, the newly synthesized compounds displayed moderate to good cytotoxicity on cervical and leukemia cancer cell lines. In addition these compounds were found to be nontoxic to normal cell (PBMCs) (IC50>50 μM). The structure-activity relationship is also discussed. The most effective anticancer compound 9 was found to be active with IC50 value of 10.6 μM. It demonstrated significant antiproliferative influence on Jurkat cell lines. The morphological changes and growth characteristics of HeLa cells treated with compound 4 were analyzed by means of SEM.
Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India. Electronic address: shamsuzzaman9@gmail.com.
Shamsuzzaman
Hena
H
Khanam
Ashraf
A
Mashrai
Asif
A
Sherwani
Mohammad
M
Owais
Nazish
N
Siddiqui
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002776:Cholestanes / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D002776:Cholestanes; D011720:Pyrazoles
Anticancer; Cholest-5-en-7-one; MTT; Pyrazolines; SEM