1201799-40-7Relevant articles and documents
New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres
Attia, Mohamed I.,Eldehna, Wagdy M.,Afifi, Samar A.,Keeton, Adam B.,Piazza, Gary A.,Abdel-Aziz, Hatem A.
, (2017)
The synthesis and molecular characterization of new isatin-based hydrazonoindolin-2-ones 4a-o and 7a-e are reported. The in vitro anti-proliferative potential of the synthesized compounds 4a-o and 7a-e was examined against HT-29 (colon), ZR-75 (breast) and A549 (lung) human cancer cell lines. Compounds 7b, 7d and 7e were the most active congeners against the tested human cancer cell lines with average IC50 values of 4.77, 3.39 and 2.37 μM, respectively, as compared with the reference isatin-based drug, sunitinib, which exhibited an average IC50 value of 8.11 μM. Compound 7e was selected for further pharmacological evaluation in order to gain insight into its possible mechanism of action. It increased caspase 3/7 activity by 2.4- and 1.85-fold between 4 and 8 h of treatment, respectively, at 10 μM and it caused a decrease in the percentage of cells in the G1 phase of the cell cycle with a corresponding increase in the S-phase. In addition, compound 7e increased phosphorylated tyrosine (p-Tyr) levels nearly two-fold with an apparent IC50 value of 3.8 μM. The 7e-loaded PLGA microspheres were prepared using a modified emulsion-solvent diffusion method. The average encapsulation efficiency of the 7e-loaded PLGA microspheres was 85% ± 1.3. While, the in vitro release profile of the 7e-loaded microspheres was characterized by slow and continuous release of compound 7e during 21 days and the release curve was fitted to zero order kinetics. Incorporation of 7e into PLGA microspheres improved its in vitro anti-proliferative activity toward the human cancer cell line A549 after 120 h incubation period with an IC50 value less than 0.8 μM.
Novel thiomorpholine tethered isatin hydrazones as potential inhibitors of resistant Mycobacterium tuberculosis
Karunanidhi, Sivanandhan,Chandrasekaran, Balakumar,Karpoormath, Rajshekhar,Patel, Harun M.,Kayamba, Francis,Merugu, Srinivas Reddy,Kumar, Vishal,Dhawan, Sanjeev,Kushwaha, Babita,Mahlalela, Mavela Cleopus
, (2021)
Novel chemotherapeutic agents against multidrug resistant-tuberculosis (MDR-TB) are urgently needed at this juncture to save the life of TB-infected patients. In this work, we have synthesized and characterized novel isatin hydrazones 4(a-o) and their thi
PHARMACEUTICAL COMPOUNDS
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Page/Page column 16, (2018/06/22)
A compound having the general formula (I) or (II), in which R, R1, R2 and R3 are as described herein, or a pharmaceutically acceptable salt thereof, is provided. An associated method for treating a mycobacterial infection is also provided.
Synthesis leishmanicidal activities of bis-Schiff bases of isatins
Khan, Momin,Khan, Khalid Mohammed,Rahim, Fazal,Samreen,Perveen, Shahnaz,Karim, Aneela,Imtiazuddin,Choudhary, Muhammad Iqbal
, p. 520 - 526 (2015/08/04)
Twenty seven (27) derivatives of bis-Schiff bases of isatins 1-27 were studied for their leishmanicidal potential. Out of twenty seven (27) analogs, five exhibited varying degree of leishmanicidal activity with IC50 values 44.86 ± 0.66, 65.27 ±
Superoxide respiratory burst inhibitory activity of bis-schiff bases of Isatins
Khan, Khalid Mohammed,Khan, Momin,Ali, Muhammad,Qadir, Muhammad Irfan,Perveen, Shahnaz,Karim, Aneela,Choudhary, Muhammad Iqbal
, p. 987 - 993 (2013/07/26)
Bis-Schiff bases 1-27 were synthesized and evaluated for their anti-inflammatory activity and possible cytotoxicity. Compounds 1-27 showed a varying degree of respiratory burst inhibitory activity with IC50 values between 242.97 - 652.12 μM. Co
Synthesis of bis-Schiff bases of isatins and their antiglycation activity
Khan, Khalid Mohammed,Khan, Momin,Ali, Muhammad,Taha, Muhammad,Rasheed, Saima,Perveen, Shahnaz,Choudhary, M. Iqbal
experimental part, p. 7795 - 7801 (2010/03/30)
Bis-Schiff bases 1-27 have been synthesized and their in vitro antiglycation potential has been evaluated. Compounds 21 (IC50 = 243.95 ± 4.59 μM), 20 (IC50 = 257.61 ± 5.63 μM), and 7 (IC50 = 291.14 ± 2.53 μM) showed an exc