26155-36-2Relevant academic research and scientific papers
Methyl-2-arylidene hydrazinecarbodithioates: Synthesis and biological activity
Mahapatra, Manojkumar,Kulandaivelu, Umasankar,Saiko, Philipp,Graser, Geraldine,Szekeres, Thomas,Andrei, Graciela,Snoeck, Robert,Balzarini, Jan,Jayaprakash, Venkatesan
, p. 650 - 656 (2013)
Methyl-2-arylidene hydrazine-carbodithioate has not been of particular interest to researchers even though its metal complexes are extensively reported on due to their biological activity. This study examined the cytostatic and antiviral activity of twelve methyl-2-arylidene hydrazinecarbodithioates reported by many researchers as intermediates for the synthesis of thiosemicarbazides and the preparation of their metal complexes. Compounds IIc, IIi, and IIl with tridentate ligand features were found to have the lowest IC50 value (6.5 μM, ≈ 1 μM, and 0.8 μM, respectively) against HL60 human promyelocytic leukemia cells. They were also most inhibitory to human embryonic lung (HEL) fibroblast proliferation (5.3 μM, 17 μM, and 2.6 μM). Compound IIc and IIl show antiviral activity against wild-type herpes simplex virus (HSV), varicella zoster virus (VZV), and acyclovirresistant HSV; however, these activities were observed at concentrations at which the compounds also markedly inhibit HL60 and HEL cell proliferation.
Synthesis antimicrobial and anticancer activity of N′- arylmethylidene-piperazine-1-carbothiohydrazide
Kulandaivelu, Umasankar,Shireesha, Boyapati,Mahesh, Chidara,Vidyasagar, Jannu Vincent,Rao, Tadikonda Rama,Jayaveera,Saiko, Philipp,Graser, Geraldine,Szekeres, Thomas,Jayaprakash, Venkatesan
, p. 2802 - 2808 (2013/07/26)
Ten newly synthesized thiosemicarbazones of piperazine (3a-3j) were evaluated for their antibacterial and antifungal activity against non-pathogenic strains of Escherichia coli (NCIM 2068), Klebsiella pneumonia (NCIM 2957), Staphylococcus aureus (NCIM 2079), and Bacillus subtilis (NCIM 2921); pathogenic strains of Vibrio cholerae, protease, Candida albicans and Aspergillus niger. All the 10 compounds (3a-3j) were found to be better than Ciprofloxacin against B. subtilis and four molecules (3c, 3d, 3e, and 3h) against S. aureus. Compound 3j, a derivative of benzophenone, has been identified as a potent and promising candidate against C. albicans. The compounds were also evaluated for their anticancer activity against HBL-100 and HL60 cell lines. Compound 3a, a p-hydroxy benzaldehyde derivative, has been identified as a potent and promising candidate.
Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives
Kulandaivelu, Umasankar,Padmini, Valisakka Gari,Suneetha, Kyatham,Shireesha, Boyapati,Vidyasagar, Jannu Vincent,Rao, Tadikonda Rama,Jayaveera,Basu, Arijit,Jayaprakash, Venkatesan
experimental part, p. 84 - 90 (2011/09/21)
Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC50 value of about 1 aμM. Compound 4f showed potent antifungal activity against Candida albicans (IC50a=a1.29 aμM) and compound 4h showed potent anticancer activity (IC50a=a0.07 aμM). Hydroxamate derivatives 4a-4l were found to show better antimicrobial and anticancer activity in compariosn with their acid counterparts 3a-3l. Copyright
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity
Chetan, Bhadaliya,Bunha, Mahesh,Jagrat, Monika,Sinha, Barij Nayan,Saiko, Philipp,Graser, Geraldine,Szekeres, Thomas,Raman, Ganapathy,Rajendran, Praveen,Moorthy, Dhatchana,Basu, Arijit,Jayaprakash, Venkatesan
supporting information; experimental part, p. 3906 - 3910 (2010/09/03)
Six compounds were synthesized with piperazine in linker region and hydroxamate as Zinc Binding Group (ZBG). They were screened against three cancer cell-lines (NCIH460; HCT116; U251). Compounds 5c and 5f with GI50 value of 9.33 ± 1.3 μM and 12.03 ± 4 μM, respectively, were tested for their inhibitory potential on hHDAC8. Compound 5c had IC50 of 33.67 μM. Compounds were also screened for their anticancer activity against HL60 human promyelocytic leukemia cell line due to the presence of pharmacophoric features of RR inhibitors in them. Compound 5c had IC 50 of 0.6 μM at 48 h.
