Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives.

Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives.

Publication date: Dec 01, 2019

Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3′-hydroxy-4′-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourteen of the new compounds were evaluated for their in vitro cytotoxic activity by National Cancer Institute (NCI) against 60 human tumour cell lines panel. The best five compounds in terms of in vitro growth inhibition were screened in the second stage five dose-response studies, three of them showing a very good antiproliferative activity with GI

Open Access PDF

Popovici, L., Amarandi, R.M., , Mangalagiu, , Mangalagiu, and Danac, R. Synthesis, molecular modelling and anticancer evaluation of new pyrrolopyridazine and pyrrolophthalazine derivatives. 24981. 2019 J Enzyme Inhib Med Chem (34):1.

Concepts Keywords
Antiproliferative Oncology
Cytotoxic Chemotherapy
Dose Response Health
Heterocyclic Antineoplastic drugs
Moiety Clinical medicine
Molecular Modelling Medicine
NCI Tumor
Ring Tumour
Structure Activity Relationship Drug Screening
Tumour Pyrrole
Phthalazine

Semantics

Type Source Name
disease MESH Cancer
disease MESH growth

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