Development of Semisynthetic Apoptosis-Inducing Agents Based on Natural Phenolic Acids Scaffold: Design, Synthesis and In-Vitro Biological Evaluation

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2022 Oct 14

PMID 36235260

Authors

Shahira M Ezzat

Heba El Sayed Teba

Inas G Shahin

Ahmed M Hafez

Aliaa M Kamal

Nora M Aborehab

Affiliations

Soon will be listed here.

Abstract

A crucial target in drug research is magnifying efficacy and decreasing toxicity. Therefore, using natural active constituents as precursors will enhance both safety and biological activities. Despite having many pharmacological activities, caffeic and ferulic acids showed limited clinical usage due to their poor bioavailability and fast elimination. Therefore, semisynthetic compounds from these two acids were prepared and screened as anticancer agents. In this study, CA and FA showed very potent anticancer activity against Caco-2 cells. Consequently, eighteen derivatives were tested against the same cell line. Four potent candidates were selected for determination of the selectivity index, where compound revealed a high safety margin. Compound represented a new scaffold and showed significant cytotoxic activity against Caco-2. Cell-cycle analysis and evaluation of apoptosis showed that derivatives , , , and showed the highest proportion of cells in a late apoptotic stage.

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