Convenient Synthesis, Characterization, Cytotoxicity and Toxicity of Pyrazole Derivatives

Abstract

The reaction of 1 with phenylisothiocyanate followed by treatment with the α-halocarbonyl compounds 24a-c afforded the thiazole derivatives 25a-c. The synthesized products were evaluated for their cytotoxicity against cancer and normal cell lines. Most compounds showed significant anticancer activity without affecting the normal fibroblast cells. The toxicity of the most pontent cytotoxic compounds was measured using Brine-Shrimp Lethality Assay.

Design, Synthesis, and Biological Evaluation of Densely Substituted Dihydropyrano[2,3-c]pyrazolesviaa Taurine-Catalyzed Green Multicomponent Approach

“…They are found to be novel selective PPARγ agonists with partial binding properties and candidates for the treatment of type II diabetes. In line, a broad scale of anticancer activity was also reported by Adibi et al and Kamel independently , The broad-scale pharmaceutical applications of pyrano­[2,3- c ]­pyrazole including its appearance in numerous biologically important scaffolds manifest its significant demand worldwide (Figure ).…”

“…In line, a broad scale of anticancer activity was also reported by Adibi et al 19 and Kamel independently. 20 In vitro anticancer activity against human liver carcinoma (HepG2), human mouth carcinoma (KB), human colon adenocarcinoma (SW48), and human lung carcinoma (A549) and reports against human gastric cancer (NUGC), human colon cancer (DLD1), human liver cancer (HA22T and HEPG2), nasopharyngeal carcinoma (HONE1), and human breast cancer (MCF) show the importance of pyranopyrazoles and its synthetic demand. 21,22 The broad-scale pharmaceutical applications of pyrano [2,3-c]pyrazole including its appearance in numerous biologically important scaffolds manifest its significant demand worldwide (Figure 1).…”

Synthesis of Metal–Organic Frameworks MIL-101(Cr)-NH2 Containing Phosphorous Acid Functional Groups: Application for the Synthesis of N-Amino-2-pyridone and Pyrano [2,3-c]pyrazole Derivatives via a Cooperative Vinylogous Anomeric-Based Oxidation

“…Also, the absorption bands observed at 1021 and 1081 cm –1 are related to the P–O bond stretching and that at 1146 cm –1 is related to PO . Furthermore, peaks of Cr–O of octahedral CrO 6 appeared at 1391 cm –1 respectively (Figure ). The FT-IR spectrum difference between MIL-101­(Cr)-NH 2 and MIL-101­(Cr)-N­(CH 2 PO 3 H 2 ) 2 confirmed the structure of the catalyst.…”

Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations

“…The cytotoxic effects of some pyrazole analogs against specific cell lines including human breast cancer cells (MDA-MB-231 and MCF-7) appear promising to the development of anticancer drugs ( Kamel, 2015 ). Compound 1 containing a distal pyrazole ring and sulphonyl moiety decreased the viability of MCF7 (IC 50 = 39.70 µM).…”