I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article 3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I & TOP II isomerases inhibitors published in 2021. Category: indole-building-block, Reprint Addresses Abdel-Aziz, M (corresponding author), Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt.; Abuo-Rahma, GEDA (corresponding author), Deraya Univ, Fac Pharm, Dept Pharmaceut Chem, New Minia, Minia, Egypt.. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde
We report herein design and synthesis of a new series of 3,7-bis-benzylidenes of ciprofloxacin. Most of the target compounds revealed good cytotoxic activity; the most potent 4e and 4i achieved strong broad spectrum antiproliferative activity with comparable activity to Doxorubicin with IC50 (M-mu) of 1.21 +/- 0.02, 0.87 +/- 0.04, 1.21 +/- 0.02; 0.41 +/- 0.02, 0.57 +/- 0.06, 1.31 +/- 0.04 and 1.26 +/- 0.01, 1.79 +/- 0.04, 0.63 +/- 0.01 against leukemia cancer cell line HL-60 (TB), colon cancer cell line HCT-116 and breast cancer cell line MCF7, respectively. Moreover, the most potent derivative 4i induced apoptosis at G2/M phase Investigating the mechanism of action of compounds 4e, 4 h and 4i exhibited promising dual TOP I alpha and TOP IIB % inhibition comparable to Camptothecin and Etoposide; respectively. Docking of 4e, 4 h and 4i into the active site of topo I and II proteins compared to Camptothein and Etoposide revealed acceptable binding score and augmented enzyme assay data. Hence, 4e and 4i are promising targeted antiproliferative dual acting TOP I alpha TOP IIB inhibitors that require further optimization.
Welcome to talk about 120-14-9, If you have any questions, you can contact Samir, M; Ramadan, M; Abdelrahman, MH; Abdelbaset, MS; Abourehab, MAS; Abdel-Aziz, M; Abuo-Rahma, GEDA or send Email.. Category: indole-building-block
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