Safety of 4′-Hydroxyacetophenone. Authors Abdel-Rahman, IM; Mustafa, M; Mohamed, SA; Yahia, R; Abdel-Aziz, M; Abuo-Rahma, GEA; Hayallah, AM in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about in [Abdel-Rahman, Islam M.; Mustafa, Muhamad; Abuo-Rahma, Gamal El-Din A.; Hayallah, Alaa M.] Deraya Univ, Fac Pharm, Dept Pharmaceut Chem, New Minia 61519, Minia, Egypt; [Mohamed, Soad A.] Deraya Univ, Fac Pharm, Dept Pharmaceut, New Minia 61519, Minia, Egypt; [Yahia, Ramadan] Deraya Univ, Fac Pharm, Dept Microbiol, New Minia 61519, Minia, Egypt; [Abdel-Aziz, Mohamed; Abuo-Rahma, Gamal El-Din A.] Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt; [Hayallah, Alaa M.] Assiut Univ, Fac Pharm, Pharmaceut Organ Chem, Assiut, Egypt; [Hayallah, Alaa M.] Sphinx Univ, Fac Pharm, Dept Pharmaceut Chem, New Assiut, Egypt in 2021, Cited 45. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4
The design, synthesis and identification of a novel series of Mannich bases of ciprofloxacin was reported. Naphthol derivatives 2a and 2b showed highly potent cytotoxic activity among the tested compounds. Compound 2a showed broad spectrum antiproliferative activity with GI(50) of 2.5-6.79 mu M with remarkable selectivity towards renal and prostate cancers with selectivity ratios ranging from 0.17 to 6.79. Independently, 2a showed outstanding activity against colon cancer HOP-92 cell lines with IC50 of 6.66 mu M while 2b showed highly potent activity against ovarian cancer cell lines with IC50 of 0.97 mu M. Results showed that 2b induced cell cycle arrest at G2/M phase and apoptosis; compound 2b showed over-expression of caspase-3 protein level (449.2 +/- 7.95) compared to doxorubicin (578.7 +/- 14.4 pg/mL). Meanwhile, compounds 2a and 2b experienced outstanding activity against both Gram-positive and Gram-negative microorganisms. Interestingly, compound 2j experienced high activity against Escherichia coli and Pseudomonas aeruginosa with MIC of 0.036 and 0.043, respectively. Compound 2d revealed 27 folds and 22 folds, respectively increasing of activity over ciprofloxacin against Staphylococcus aureus and MRSA(reference strain). Compound 2d showed high activity against Staphylococcus aureus, MRSA (reference strain) and MRSA (clinical strain) with MIC of 0.57, 0.52, 0.082 mu g/mL, respectively. Interestingly, the most active tested compounds were found to have promising physicochemical and drug likeness properties. The Mannich bases 2j, 2d and 2g showed promising antibacterial activities, while naphthols 2a and 2b showed promising antiproliferative and antibacterial activities that require further optimization.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles