67291-72-9Relevant academic research and scientific papers
Synthesis and preliminary biological evaluation of polyamine-aniline acridines as P-glycoprotein inhibitors
Wang, Jianhong,Cheng, Pengfei,Luo, Tianwei,Wang, Zhaoyi,Zhang, Yahong,Zhao, Jin
, p. 506 - 511 (2014/06/23)
We have synthesized a series of polyamine-based anilinoacridine derivatives. The preliminary biological evaluation indicated that the 9-anilinoacridine-polyamine derivatives had low or insignificant in vitro cytotoxicity against K562 cell line and K562/ADM, the drug-resistant cell line. However, the evaluation for P-gp modulation showed that they held potent P-gp inhibitory ability. Among them, the effect of compound 7c on P-gp was even greater than that of Verapamil, the known P-gp modulator. The results suggest that 9-anilinoacridine-polyamine derivatives can be employed as effective P-gp modulators.
Synthesis, structure-activity relationship and biological activity of acridine derivatives as potent mdr-reversing agents
Wang, Jianhong,Luo, Tianwei,Li, Shaobin,Zhhang, Yahong,Wang, Chaojie,Zhao, Jin
, p. 4070 - 4079 (2013/12/04)
Multidrug resistance (MDR) mediated by P-glycoprotein is one of the best characterized transporter-mediated barriers to successful cancer chemotherapy. In an attempt to find MDR-reversing agents, a series of novel acridine derivatives were synthesized and evaluated for their in vitro antiproliferative activities against K562 and K562/ADM cells. Some of these compounds showed superior MDR-reversing activities than Amsacrine, the reference compound. Structureactivity relationships (SAR) of these compounds indicated that the N, N-diethylamine moiety had an affect on the in vitro antiproliferative activity. Interestingly, the compounds bearing N, N-diethylamine moiety showed higher growthinhibitory activity against K562/ADM cells than K562 cells. The high duplex DNA binding affinity and inhibition of topoisomerase of these acridine compounds are maintained which were confirmed by fluorescent quenching and DNA topoisomerase II cleavage assay, respectively. Moreover, several compounds were examined for their ability to increase the accumulation of rhodamine 123 in K562 and K562/ADM cells, and the result suggested that they may be inhibitors for P-glycoprotein. Our study suggested that acridine framework is a potentially interesting scaffold for developing novel MDR-reversing agents.
2-AMINOPYRIMIDINE AND 2-AMINOPYRIDINE-4-CARBAMATES FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES
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Page 67, (2010/02/10)
The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula (1) and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.
SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 67, (2010/02/11)
The present invention relates to hydroxybenzimidazole pyrimidines or pyridines or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
Synthesis of Some New 3-Methoxy-4-acylaminophenylisothiocyanates, 4'-Isothiocyanatophenoxyacetamides/Isobutyramides as Possible Anthelmintic Agents
Shridhar, D. R.,Rao, K. Srinivasa,Singh, A. N.,Rastogi, K.,Jain, M. L.
, p. 1277 - 1280 (2007/10/02)
A number of new 3-methoxy-4-acylaminophenylisothiocyanates (II and III), 4'-isothiocyanatophenoxyacetamides (IV) and 4-isothiocyanatophenoxyisobutyramides (V) have been synthesized and tested for anthelmintic, antiamoebic and antitrichomonal activities.
Activities of 2-carboxanilido 3-hydroxybenzo[b]thiophens against molluscs Biomphalaria
Gayral,Buisson,Royer
, p. 187 - 189 (2007/10/02)
The title compounds are shown to be nearly as active against molluscs as Niclosamide when they are either dihalogenated or monohalogenated and mononitrated on the benzene ring.
