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Nowadays, heterocyclic compounds act as a scaffold and are the backbone of medicinal
chemistry. Among all of the heterocyclic scaffolds, 1,4-Dihydropyridine (1,4-DHP) is one of the most
important heterocyclic rings that possess prominent therapeutic effects in a very versatile manner and
plays an important role in synthetic, medicinal, and bioorganic chemistry. The main aim of the study is
to review and encompass relevant studies related to 1,4-DHP and excellent therapeutic benefits of its
derivatives. An extensive review of Pubmed-Medline, Embase and Lancet’s published articles was
done to find all relevant studies on the activity of 1,4-DHP and its derivatives. 1,4-DHP is a potent
Voltage-Gated Calcium Channel (VGCC) antagonist derivative which acts as an anti-hypertensive, anti-
anginal, anti-tumor, anti-inflammatory, anti-tubercular, anti-cancer, anti-hyperplasia, anti-mutagenic,
anti-dyslipidemic, and anti-ulcer agent. From the inferences of the study, it can be concluded that the
basic nucleus, 1,4-DHP which is a voltage-gated calcium ion channel blocker, acts as a base for its derivatives
that possess different important therapeutic effects. There is a need of further research of this
basic nucleus as it is a multifunctional moiety, on which addition of different groups can yield a better
drug for its other activities such as anti-convulsant, anti-oxidant, anti-mutagenic, and anti-microbial.
This review would be significant for further researches in the development of several kinds of drugs by
representing successful matrix for the medicinal agents.