Synthesis and In Vitro Antitumor Activity of Novel Fluorine Containing Pyrazoles and Pyrazolines

Abstract

The present anticancer research demands more potent anticancer agents with fewer side effects than the existing ones. A series of novel substituted thiazole and benzothiazole containing nitrogen mustards (5-8; 15-17; 22-23) were synthesized and the structures of the compounds were analyzed by IR, NMR and mass spectras. Their in-vitro cytotoxicity against human lung carcinoma (A549) was investigated by MTT Assay. The compounds 16, 8 showed promising activity against A549 human lung carcinoma cell lines with % CPI 52 (More than Cisplatin) and 45.9 respectively. The DNA binding properties of the compounds were also evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compounds 22 and 5 showed the highest binding affinity with binding constant (Ki) 48.34 and 41.8 respectively.

Synthesis and Biological Evaluation of Pyrazoline and Pyrrolidine‐2,5‐dione Hybrids as Potential Antitumor Agents

“…Earlier we had reported diaryl pyrazolines with remarkable anticancer activity against MCF7 (Breast), HOP62 (lung), A498 (Renal) and MIAPACA2 (pancreatic) cell lines (Figure ). Thus, based on our past experience with this scaffold and literature evidences cited above, we selected diaryl pyrazoline as one portion of hybrid.…”

Design, in silico studies, synthesis, and in vitro anticancer assessment of new naphthylidene isoxazolidinedione derivatives

“…[5][6][7][8][9][10][11][12][13][14][15] However, we also published compounds without the TZD nucleus showing good antiproliferative activity (Figure 1). [16][17][18][19][20][21][22][23][24][25] Interestingly, there are countless pieces of literature demonstrating compounds with anticancer activity incorporating various heterocyclic rings. 17,19,[25][26][27][28][29][30] On a similar path, we have recently reported new small molecules incorporating heterocyclic rings, imidazolidinedione, and pyrrolidinedione showing excellent antitumor activity.…”

Synthesis and pharmacological evaluation of some new fluorine containing hydroxypyrazolines as potential anticancer and antioxidant agents

“…Recently Sharma et al, reported synthesis and in vitro antitumor activity of novel fluorine containing pyrazoles and pyrazolines. These compounds exhibited excellent cytotoxicity against MCF-7 breast cancer cell line [29]. Sarojini and co-workers revealed that fluorine containing hydroxypyrazolines showed potential antiproliferative activity [30].…”