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1.
J Org Chem ; 83(17): 9890-9901, 2018 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-30106298

RESUMO

Substrate-controlled generation of 3-sulfonylated 1-indenones and 3-arylated ( Z)-indenes through radical cyclization cascades of o-alkynylbenzonitriles with sulfonyl hydrazides was established by combining copper(II) with tert-butyl hydroperoxide (TBHP) as a catalytic oxidative system. With the installation of the aryl group (R1) into the alkynyl unit, sulfonyl radicals triggered addition-cyclization cascades to access 3-sulfonylated 1-indenones with good yields by using a Cu/TBHP system, whereas a series of new functionalized 3-arylated ( Z)-indenes were obtained in good yields when o-alkynylbenzonitriles bearing the alkyl group in the alkynyl unit were subjected with arylsulfonyl hydrazides with an electron-rich nature under the above conditions.

2.
Environ Toxicol Pharmacol ; 46: 270-276, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27522546

RESUMO

Although numerous hypotheses have been proposed to prevent chemotherapy-induced alopecia (CIA), effective pharmaceuticals have yet to be developed. In our study, the back hairs of C57BL/6 mice were factitiously removed. These mice were then treated with cedrol or minoxidil daily. Mice with early-stage anagen VI hair follicles were treated with cyclophosphamide (CYP, 125mg/kg) to induce alopecia. The CYP-damaged hair follicles were observed and quantified by using a digital photomicrograph. The results demonstrated that the minoxidil-treated mice suffered from complete alopecia similar to the model 6days after CYP administration. Simultaneously, the cedrol-treated (200mg/kg) mice manifested mild alopecia with 40% suppression. Histological observation revealed that anagen hair follicles of the cedrol-pretreated mice (82.5%) likely provided from damage compared with the sparse and dystrophic hair follicles of the model mice (37.0%). Therefore, the use of topical cedrol can prevent hair follicle dystrophy and provide local protection against CIA.


Assuntos
Alopecia/prevenção & controle , Antineoplásicos Alquilantes/toxicidade , Ciclofosfamida/toxicidade , Terpenos/uso terapêutico , Alopecia/induzido quimicamente , Animais , Cupressaceae/química , Dermatite de Contato/etiologia , Dermatite de Contato/imunologia , Modelos Animais de Doenças , Feminino , Folículo Piloso/efeitos dos fármacos , Folículo Piloso/crescimento & desenvolvimento , Folículo Piloso/patologia , Camundongos Endogâmicos C57BL , Folhas de Planta/química , Sesquiterpenos Policíclicos , Pele/efeitos dos fármacos , Pele/imunologia , Terpenos/administração & dosagem , Terpenos/isolamento & purificação , Terpenos/toxicidade , Testes de Toxicidade Aguda
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