Microwave-assisted Phospha-Michael addition reactions in the 13α-oestrone series and <i>in vitro</i> antiproliferative properties
نویسندگان
چکیده
Microwave-assisted phospha-Michael addition reactions were carried out in the 13α-oestrone series. The exocyclic 16-methylene-17-ketones as α,β-unsaturated ketones reacted with secondary phosphine oxides nucleophilic partners. furnished two tertiary oxide diastereomers high yields. main product was 16α-isomer. antiproliferative activities of newly synthesised organophosphorus compounds against a panel nine human cancer cell lines investigated by means MTT assays. most potent compound, diphenylphosphine derivative 3-O-methyl-13α-oestrone series (9), exerted selective growth-inhibitory activity UPCI-SCC-131 and T47D low micromolar IC50 values. Moreover, it displayed good tumour selectivity property determined non-cancerous mouse fibroblast cells.
منابع مشابه
Atmospheric pressure microwave assisted heterogeneous catalytic reactions.
The purpose of the study was to investigate microwave selective heating phenomena and their impact on heterogeneous chemical reactions. We also present a tool which will help microwave chemists to answer to such questions as "My reaction yields 90% after 7 days at reflux; is it possible to obtain the same yield after a few minutes under microwaves?" and to have an approximation of their reactio...
متن کاملMicrowave assisted reactions of some azaheterocylic compounds.
A fast, general, environmentally friendly and facile method for preparation of five- and six-membered ring diazaheterocylic salts under microwave irradiation is presented. The N-alkylation reactions of imidazole, pyrimidine, pyridazine and phthalazine have been studied. The microwaves remarkably accelerated these N-alkylations, the reaction times decreased dramatically, the reaction conditions ...
متن کاملMicrowave-assisted synthesis of new selenazole derivatives with antiproliferative activity.
New aryl-hydrazinyl-1,3-selenazole and aroyl-hydrazonyl-1,3-selenazoles were synthesized via Hantzsch type condensation reactions of selenosemicarbazides with α-halogenocarbonyl derivatives, under classical versus microwave heating conditions. Excellent yields and shorter reaction times were obtained under irradiation conditions. The structures of the synthesized compounds were assigned based o...
متن کاملlearners’ attitudes toward the effectiveness of mobile-assisted language learning (mall) in vocabulary acquisition in the iranian efl context: the case of word lists, audiobooks and dictionary use
رشد انفجاری تکنولوژی فرصت های آموزشی مهیج و جدیدی را پیش روی فراگیران و آموزش دهندگان گذاشته است. امروزه معلمان برای اینکه در امر آموزش زبان بروز باشند باید روش هایی را اتخاذ نمایند که درآن ها از تکنولوژی جهت کمک در یادگیری زبان دوم و چندم استفاده شده باشد. با در نظر گرفتن تحولاتی که رشته ی آموزش زبان در حال رخ دادن است هم اکنون زمان مناسبی برای ارزشیابی نگرش های موجود نسبت به تکنولوژی های جدید...
15 صفحه اولPreparation and double Michael addition reactions of a synthetic equivalent of the Nazarov reagent.
A synthetic equivalent of the Nazarov reagent, the silyl derivative 2, able to undergo base-catalyzed double Michael addition reactions with α,β-unsaturated carbonyl compounds has been developed. The new reagent satisfactorily reacts with unsaturated indolo[2,3-a]quinolizidine lactams to give pentacyclic yohimbinone-type derivatives.
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: ['1475-6374', '1475-6366']
DOI: https://doi.org/10.1080/14756366.2021.1963241