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Croatica Chemica Acta, Vol. 94 No. 4, 2021.

Original scientific paper

https://doi.org/10.5562/cca3859

A Novel Class of Pyrazoline Analogue of Combretastatin-A4 (CA-4): Synthesis Characterization and in-vitro Biological Testing

Sadanand N. Shringare orcid id orcid.org/0000-0003-2217-5648 ; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Punyashlok Ahilyadevi Holkar Solapur University, Solapur, Maharashtra, 413255, India
Pravin S. Bhale orcid id orcid.org/0000-0003-3639-0357 ; Department of Chemistry, Yeshwantrao Chavan Mahavidyalaya, Tuljapur-413 601, Maharashtra, India
Hemant V. Chavan ; Department of Chemistry, A.S.P. College Devrukh (Autonomous), Dist-Ratnagiri-415804, Maharashtra, India
Purva L. Hundekari ; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Punyashlok Ahilyadevi Holkar Solapur University, Solapur, Maharashtra, 413255, India
Makarand A. Kulkarni ; Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Punyashlok Ahilyadevi Holkar Solapur University, Solapur, Maharashtra, 413255, India

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Abstract

A series of pyrazoline bridged combretastatin analogues were designed and synthesised from their precursor chalcone analogues, and all these compounds were ascertained by IR, 1H NMR, and mass spectral analysis. Subsequently, all these compounds were evaluated for anticancer activities against breast cancer (MCF-7) and normal Vero (Monkey Kidney) cell lines, and five selected compounds from the series were evaluated against Hela (Human Cervical), MDA-MB-231 (Breast), and A-549 (Lung cancer) cell lines using the Sulforhodamine B (SRB) assay method. Compounds 3a, 6a, 6e, 5b, 7a, 5a, and 7d were found to be the most potent in the series, with a GI50 value of 10 to 30 M in the MCF-7 cell line. Moreover, the same compounds 6a and 7a showed remarkable cytotoxicity against the A-549 (Lung) cell line with a GI50 value ranging from 10 to 30 M, while compound 3a displayed moderate cytotoxicity against the Hela (Human Cervical) cell line. All these compounds were found nontoxic to the Vero (Monkey Kidney) normal cell line.

Keywords

anticancer; cytotoxicity; pyrazoline; combretastatin

Hrčak ID:

281184

URI

https://hrcak.srce.hr/281184

Publication date:

8.8.2022.

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