In 2021 J MOL STRUCT published article about THIOUREA DERIVATIVES BEARING; ANTITUMOR-ACTIVITY; INHIBITORY-ACTIVITY; CANCER; SENSITIVITY; MOIETY in [Abd El-Meguid, Eman A.] Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Dept Chem Nat & Microbial Prod, Cairo 12622, Egypt; [Moustafa, Gaber O.] Natl Res Ctr, Chem Ind Res Div, Peptide Chem Dept, Cairo 12622, Egypt; [Awad, Hanem M.] Natl Res Ctr, Dept Tanning Mat & Leather Technol, Cairo 12622, Egypt; [Zaki, Eman R.] Natl Res Ctr, Dept Mol Biol, Cairo 12622, Egypt; [Nossier, Eman S.] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Med Chem, Cairo 11754, Egypt in 2021, Cited 47. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Name: Benzoic anhydride
Novel benzo[d] thiazole-based analogues were synthesized with the aim of screening their in vitro anticancer activity. All the new derivatives 4-21 were evaluated against human hepatocellular carcinoma (HepG-2) and breast cancer cells (MCF-7) using doxorubicin as a reference drug. All compounds exhibited excellent potency against MCF-7 (IC50 values ranging from 0.71 +/- 0.4 to 1.04 +/- 0.7 mu M) and variable promising potency against HepG-2 (IC50 ranged from 2.53 +/- 2.5 to 3.47 +/- 3.4 mu M) comparing with the standard (IC50 = 1.03 +/- 0.8 mu M and 2.85 +/- 1.9 mu M, respectively) in addition to their safety towards the normal cell line. Compounds 5, 6, 7, 13 and 16 having the highest cytotoxic activity, were further evaluated for their EGFR inhibitory activity using Erlotinib as a reference drug. Molecular docking studies were performed for the promising compounds 5, 6 and 7 to interpret their detected enzymatic activities based upon their binding interactions with the receptor. Moreover, cell cycle analysis and detection of apoptosis induction illustrated that compounds 5 and 6 exhibited a significant pre G(1) and G(2)/M cell cycle arrest, in comparison with the untreated MCF-7 cells. In addition, compounds 5 and 6 elevated the levels of the oncogenic parameters; Bax, p53 and caspase-3 with decreased level of Bcl-2. These previous encouraging results of biological evaluation of the newly synthesized benzothiazoles could recommend an excellent framework toward the detection of new potent antitumor leads. (C) 2021 Elsevier B.V. All rights reserved.
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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com