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Substituted chloroacetamides as potential cancer stem cell inhibitors: Synthesis and biological evaluation.

Abstract

Cancer kills, irrespective of geographical and cultural origin. Novel modalities for treating cancer are desperately needed. Cancer stem cells (CSCs), main culprits behind chemoresistance and tumor relapse, are one of the few logical choices. Herein, we report the synthesis and biological evaluation of small molecules with chloroacetamide war-head. These molecules were screened for viability against various breast, prostate, and oral cancer cell lines using MTT and soft-agar assays. Further, promising hits were screened in sphere-forming assay with the aim of discovering potential anti-CSC agents. Our optimism yielded four hits inhibiting self-renewal of cancer cells with stem-like characters in vitro. Finally, the hits were evaluated for in vitro toxicity against human peripheral blood mononuclear cells and mouse embryonic fibroblast cell line. Overall, these preliminary investigations yielded three hits exhibiting promising anti-CSC potential with little or no toxicity against normal cells.

Authors+Show Affiliations

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Mumbai, India.Department of Cancer Biology, Godavari Biorefineries Ltd., Mumbai, India.Department of Cancer Biology, Godavari Biorefineries Ltd., Mumbai, India.Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Mumbai, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31800121

Citation

Padhariya, Komal N., et al. "Substituted Chloroacetamides as Potential Cancer Stem Cell Inhibitors: Synthesis and Biological Evaluation." Drug Development Research, 2019.
Padhariya KN, Athavale M, Srivastava S, et al. Substituted chloroacetamides as potential cancer stem cell inhibitors: Synthesis and biological evaluation. Drug Dev Res. 2019.
Padhariya, K. N., Athavale, M., Srivastava, S., & Kharkar, P. S. (2019). Substituted chloroacetamides as potential cancer stem cell inhibitors: Synthesis and biological evaluation. Drug Development Research, doi:10.1002/ddr.21628.
Padhariya KN, et al. Substituted Chloroacetamides as Potential Cancer Stem Cell Inhibitors: Synthesis and Biological Evaluation. Drug Dev Res. 2019 Dec 4; PubMed PMID: 31800121.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Substituted chloroacetamides as potential cancer stem cell inhibitors: Synthesis and biological evaluation. AU - Padhariya,Komal N, AU - Athavale,Maithili, AU - Srivastava,Sangeeta, AU - Kharkar,Prashant S, Y1 - 2019/12/04/ PY - 2019/08/09/received PY - 2019/10/24/revised PY - 2019/11/09/accepted PY - 2019/12/5/entrez PY - 2019/12/5/pubmed PY - 2019/12/5/medline KW - CSCs KW - breast cancer KW - cancer stem cells KW - chloroacetamides KW - oral cancer KW - prostate cancer KW - soft-agar assay KW - sphere-forming assay JF - Drug development research JO - Drug Dev. Res. N2 - Cancer kills, irrespective of geographical and cultural origin. Novel modalities for treating cancer are desperately needed. Cancer stem cells (CSCs), main culprits behind chemoresistance and tumor relapse, are one of the few logical choices. Herein, we report the synthesis and biological evaluation of small molecules with chloroacetamide war-head. These molecules were screened for viability against various breast, prostate, and oral cancer cell lines using MTT and soft-agar assays. Further, promising hits were screened in sphere-forming assay with the aim of discovering potential anti-CSC agents. Our optimism yielded four hits inhibiting self-renewal of cancer cells with stem-like characters in vitro. Finally, the hits were evaluated for in vitro toxicity against human peripheral blood mononuclear cells and mouse embryonic fibroblast cell line. Overall, these preliminary investigations yielded three hits exhibiting promising anti-CSC potential with little or no toxicity against normal cells. SN - 1098-2299 UR - https://www.unboundmedicine.com/medline/citation/31800121/Substituted_chloroacetamides_as_potential_cancer_stem_cell_inhibitors:_Synthesis_and_biological_evaluation L2 - https://doi.org/10.1002/ddr.21628 DB - PRIME DP - Unbound Medicine ER -