- NSCLC structure-activity relationship (sar) study of diisothiocyanates for antiproliferative activity on A549 Human non-small cell lung carcinoma (NSCLC)
-
Isothiocyanate functional group (-N=C=S) is widely accepted as an important moiety for anti-cancer effects of naturally occurring isothiocyanate compounds (ITCs). Herein, a series of diisothiocyanate (diITCs) derivatives were synthesized and evaluated in antiproliferative assays on A549 human non-small cell lung cancer and IMR90 human foetal lung cell lines for structure-activity relationship (SAR) and cancer cell selectivity studies. Results showed that aliphatic and benzylic diITCs were more cytotoxic to A549 cells than natural ITCs; benzyl isothiocyanate (BITC) and phenyl isothiocyanate (PITC), and a currently available anticancer drug; etoposide. Aromatic diITCs were not as active. Notably, most of the diITCs reported in this work were significantly more selective than etoposide to inhibit proliferation of the cancer cells (A549) over the normal cells (IMR90). This study demonstrated a guideline to modify chemical structures of diITCs for anti-NSCLC agents.
- Chatwichien, Jaruwan,Prachavna, Buntarika,Suntivich, Rinrada,Kumphune, Sarawut
-
p. 569 - 574
(2019/08/07)
-
- Dapson in heterocyclic chemistry, part I: Novel synthesis of sulfone biscompounds for antimicrobial and antitumor activities
-
This article describes the synthesis of some novel sulfone bis-compounds bearing the biologically active thioether 3-6; thioureido 7, 8, 15, 16; triazole 10, 11; thiosemicarbazido 9, 12, 13; and 1,3,4-thiadiazole 14, 17 moieties starting with 4,4′-diisoth
- Ghorab,Taha,Radwan,Amin,Shehab,Faker
-
experimental part
p. 2891 - 2905
(2009/09/06)
-
- Dapson in heterocyclic chemistry, part II: Antimicrobial and antitumor activities of some novel sulfone biscompounds containing biologically active thioureido, carbamothioate, quinazoline, imidazolidine, and thiazole moieties
-
The reaction of 4,4′-diisothiocyanato-1,1-diphenylsulfone 2 with aromatic amines and phenol derivatives afforded the corresponding thioureio derivatives 3-9, respectively. Also, the reaction of 2 with catechol gave the corresponding carbamothioate derivat
- Ghorab,Radwan,Taha,Amin,Shehab,Faker
-
body text
p. 2906 - 2917
(2009/09/06)
-
- Dapson in heterocyclic chemistry, part III: Synthesis, antimicrobial, and antitumor activities of some new bisheterocyclic compounds containing biologically active diphenylsulfone moiety
-
The key intermediate diisothiocyanate 2 was allowed to react with 5-amino-3-methyl-pyrazole-4-carbonitrile 3, ethyl 5-amino-1-phenyl-pyrazole-4- carboxylate 6, 2-amino-tetrahydrobenzo[b]thiophene-3-car-bonitrile 9, ethyl-2-amino-tetra-hydrobenzo[b]thiophe
- Ghorab,Amin,El Gaby,Taha,Shehab,Faker
-
body text
p. 2918 - 2928
(2009/09/25)
-
- Rapid synthesis of 2-cyanobenzothiazole, isothiocyanate and cyanoformanilide derivatives of dapsone
-
The rapid synthesis of 2-cyanobenzothiazole, isothiocyanate and cyanoformanilide derivatives of dapsone was examined. The derivatives of the leprostatic drug dapsone were prepared by way of imino-1,2,3-dithiazoles obtained by condensation of aromatic prim
- Besson, Thierry,Guillard, Jerome,Rees, Charles W.
-
p. 563 - 566
(2007/10/03)
-