Abstract
Objective: In this study, a series of novel 2,3-disubstituted quinazolines (4a-4l) were synthesized using standard procedures and elucidated through different spectroscopic techniques.
 Methods: Obtained compounds were evaluated for their cytotoxicity against human breast cancer (MDA-MB-231) and ovarian cancer (SK-O-V3) cell lines using MTT assay. Docking studies with JAK2 protein were performed to elucidate the possible mechanistic insights into these novel quinazoline derivatives.
 Results: Moderate-to-good in vitro cytotoxic potentials of the newly synthesized molecules were reported against selected human cancer cell lines. Among the tested molecules, compound 4e showed good cytotoxic activity against MD-AMB-231 (14.2 ± 0.86 μM) and against SK-O-V3 (17.7 ± 0.62 μM).
 Conclusion: The in vitro studies of the newly synthesized quinazoline derivatives reported considerable cytotoxic potentials against both breast and ovarian cancer cell lines and SAR studies suggest that quinazoline derivatives with heterocyclic benzothiazole nucleus with hydrophilic acetamide linkage at the 3rd position could probably increase the cytotoxic potentials and the presence of chlorine substitution could add more benefit. With the reported bioactivities of these derivatives, further studies on the derivatization could elucidate the broader cytotoxic potentials.
Highlights
Cancer is a major public health problem worldwide and is the leading cause of deaths to 606,880 alone in the USA in 2019 alone
Mass spectra of the synthesized compounds were recorded on a Shimadzu liquid chromatography–mass spectrometry (LCMS)-8030 using ESI mode
Chemistry Twelve new compounds of 2-substituted quinazolines and 2,3-disubstituted quinazolines were synthesized and the reaction sequence for the synthesis of these compounds is outlined in Scheme 1
Summary
Cancer is a major public health problem worldwide and is the leading cause of deaths to 606,880 alone in the USA in 2019 alone. Majority of cancer deaths are due to cancer of lungs, breast, genital system, digestive system, lymphoma, leukemia, etc. Breast cancer is one of the major problems in women leads to enhance mortality rate. In 2019, the American Cancer Society estimated 271,270 cases of the invasive breast cancer diagnosed and 42,260 deaths in the U. Advancement in chemotherapeutic strategies is currently not efficient in treating the malignancy, due to the lack of selectivity between normal cell and cancer cell, due to the development of drug resistance resulting in poor clinical benefits. There is a necessity to develop novel molecules to treat wide variety of cancers that are occurring
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