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At least 307 records · Page 17Linked to original sources
PubMed1993

Chloroquinoxaline sulfonamide: a sulfanilamide antitumor agent entering clinical trials.

Chloroquinoxaline sulfonamide (CQS) has been developed to the clinical trial stage based on its activity in the Human Tumor Colony Forming Assay (HTCFA). In the HTCFA, CQS demonstrated inhibition of colony formation against breast, lung, melanoma and ovarian carcinomas. The mechanism of action of CQS is unknown. It does not appear to inhibit folate metabolism as does the structurally similar sulfaquinoxaline. Preclinical toxicology studies in dogs and rats have shown that CQS is toxic to lymphoid organs, bone marrow, gastrointestinal tract, pancreas, CNS, adrenal glands and testes. Toxicity was generally reversible with the exception of testicular atrophy in dogs and rats which occurred late and was not reversible within the study time frame. The pharmacokinetic data indicate that CQS binds to serum proteins in a dose and species specific manner. Terminal half-lives appear to vary between species from 60 hours in mice, 15 hours in rats, and 45-132 hours in dogs. Preliminary data indicate a longer terminal half-life in humans. Two phase I trials are ongoing using a 60 min infusion schedule once every 28 days. The starting dose for each trial was 18 mg/m2.

Animals↗
PubMed1996

Cobalt(II), nickel(II), and copper(II) complexes of sulfanilamide derivatives: synthesis, spectroscopic studies, and antibacterial activity. Crystal structure of [Co(sulfacetamide)2(NCS)2].

The synthesis and characterization of new coordination compounds of Co(II), Ni(II), and Cu(II) with sulfacetamide (N-[4-(amino-fenil)sulfonil]acetamide) is reported. The complex [Co(sulfacetamide)2(NCS)2] crystallizes in the triclinic space group P-1. The cell dimensions are a = 7.80(2) A, b = 8.327(9) A, c = 9.568(3) A, alpha = 90.5(1) degrees, beta = 90.5(1) degrees, gamma = 97.8(2) degrees, V = 616(1) A3, Z = 2, and Dx = 1.689 g/cm3. The final conventional R-factor = 0.039 (Rw = 0.039) for 3535 "observed" reflections and 173 variables. The Co(II) is surrounded in a regular octahedral arrangement by two Nthyocianato from the NCS, two Namino and two Oacetamido atoms from the sulfacetamide. Each sulfacetamide, acting as a bidentate ligand, chelates two Co(II) ions as a bridge through the Namino and the Oacetamido atoms. IR, Reflectance Diffuse, EPR, and magnetic properties of the obtained complexes are discussed. The complexes were screened for their activity against E. Coli and S. aureus, showing an appreciable antimicrobial activity compared with the ligands.

Anti-Bacterial Agents↗
PubMed2004

Synthesis and antitubulin activity of N1- and N4-substituted 3,5-dinitro sulfanilamides against African trypanosomes and Leishmania.

Thirty analogues of N(1)-phenyl-3,5-dinitro-N(4),N(4)-di-n-propylsulfanilamide (GB-II-5, compound 3), a new antikinetoplastid antimitotic agent, have been synthesized and evaluated. The addition of simple functional groups to the N1 aromatic ring generally decreases antiparasitic and antimitotic potency, but placement of a dibutyl substituent at the N4 nitrogen to give N(1)-phenyl-3,5-dinitro-N(4),N(4)-di-n-butylsulfanilamide (compound 35) augments antitrypanosomal and antileishmanial activity. Compound 35 possesses IC(50) values of 0.12 and 2.6 microM against cultured T. brucei and L. donovani amastigote-like forms, surpassing the activity of compound 3 against these parasites by 3.4- and 1.9-fold, respectively. Compound 35 inhibits the assembly of leishmanial tubulin with an IC(50) of 6.9 microM and displays antimitotic effects in cultured T. brucei as assessed by flow cytometry, but shows little effect on purified mammalian tubulin, and displays 100-fold selectivity for trypanosomes over two mammalian cell lines. Although 3 and 35 were not effective in initial in vivo antitrypanosomal assays, the in vitro potency and selectivity of these compounds make N(1)-aryl-3,5-dinitro-N(4),N(4)-dialkylsulfanilamides a promising new class of antikinetoplastid agents that act on parasite tubulin.

Animals↗