6-Iodo-3h-quinazolin-4-one (16064-08-7)

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6-Iodo-3h-quinazolin-4-one(16064-08-7) video

The 6-Iodoquinazolin-4-one, with the CAS registry number (16064-08-7), is also known as 6-Iodoquinazolin-4(1H)-one. It belongs to the product category of Pharmacetical. this chemical can be prepared by 2-Amino-5-iodo-benzoic acid with Essigsaeure, Formamid. The reaction occurs with reagent ethanol and other condition of heating for 2 hours. The yield is 87 %.New series of 3-(3-trifluoromethylphenyl)-6-iodo-4(3H)-quinazolinone derivatives bearing thiosemicarbazones, pyrazoles, azomethine moieties at C-2 were synthesized. The obtained products were screened for their expected anticancer activity against; human liver cancer cell line (HepG2), breast cancer cell line (MCF-7) and human lung adenocarcinoma epithelial cell line (A549) tumor cell lines. Cytotoxicity of the synthesized compounds showed good IC50 for some products in comparison with the standard drug, doxorubicin. On the other hand, antiviral activity of the synthesized products against H5N1 showed moderate to weak activity compared to Zanamivir reference drug. 2-Aminoquinazolin-4(3H)-ones were previously discovered as perspective leads for antimalarial drug development targeting the plasmepsins. Here we report the lead optimization studies with the aim to reduce inhibitor lipophilicity and increase selectivity versus the human aspartic protease Cathepsin D. Exploiting the solvent exposed area of the enzyme provides an option to install polar groups (R1) the 5-position of 2-aminoquinazolin-4(3H)-one to inhibitors such as carboxylic acid without scarifying enzymatic potency. Moreover, introduction of R1 substituents increased selectivity factors of compounds in this series up to 100-fold for Plm II, IV vs CatD inhibition. The introduction of flap pocket substituent (R2) at 7-postion of 2-aminoquinazolin-4(3H)-one allows to remove Ph group from THF ring without notably impairing Plm inhibitory potency. Based on these findings, inhibitors were developed, which show Plm II and IV inhibitory potency in low nanomolar range and remarkable selectivity against Cathepsin D along with decreased lipophilicity and increased solubility.Among the 3-(2,6-dimethylphenyl)quinazolinone series, the introduction of an indol-5-yl substituent at the pyrazolo[3,4-d]pyrimidine 3-position led to a potent and selective PI3Kδ (IC50 = 8.6 nM) inhibitor 10d, that was more than 3630-fold, 390-fold and 40-fold selective for PI3Kδ over PI3Kα β and γ while the substitution with a 3,4-dimethoxyphenyl resulted in a potent and selective dual PI3Kδ/γ inhibitor 10e with IC50 values of 8.4 nM and 62 nM against PI3Kδ and PI3Kγ respectively. Compound 10e was also more than 1400-fold, 820-fold selective for PI3Kδ over PI3Kα and PI3Kβ. In agreement with their remarkable PI3Kδ inhibitory activity, compounds 10d and 10e showed high antiproliferative activity against human B-cell SU-DHL-6 cells. Moreover, the dual PI3Kδ/γ inhibitor 10e had reasonable pharmacokinetic profiles with a good plasma exposure, low clearance, low volume distribution, and an acceptable oral bioavailability of 34.9percent.

6-Iodo-3h-quinazolin-4-one(16064-08-7) Specifications

CAS 16064-08-7
CAS Min% 95.0
CAS Max% 100.0
Tau MDL MFCD00460007
Ki te KAUPAPA KI PUGXMZKDRVGIHC-UHFFFAOYSA-N
Ingoa Toiina, Rauemi ranei 6-Iodo-3h-quinazolin-4-kotahi
Hauira Purapura Motuhēhē
Puka Puka Kari-Maama
Packaging Pounamu tio
Tātai rāpoi C8H5IN2O
Taumaha Taumaha (g / mol) 272.04
Tuhinga o mua C1 = CC2 = C (C = C1I) C (= O) N = CN2
Tae He Maama Raro Whero Whero Whero Whero-Whero
Ko te Whakakuku 271 ° C (pan.)
anga matou ≥97.0%

6-Iodo-3h-quinazolin-4-one (16064-08-7) Te Haumaru me te Whakaaetanga

(16064-08-7) Te whakaahuatanga haumaru:

◆ H315-H319-H335

◆ Ka meinga te mamae o te kiri.

◆ Ko te ahua kino o te kanohi.

◆ Ka meinga pea e koe te ahuareka o te manawa.

(16064-08-7) Te korero whakatupato:

◆P261-P280-P305+P351+P338-P304+P340-P405-P501a
◆ Ahanoa i te pupuhi i te puehu / te paraoa / te hau / te kohu / te pupuhi / te pupuhi.
◆ Te mau kakahu maru / te tiaki / te tiaki kanohi / kanohi.
◆ MI TE KAUPAPA: Whakakotahitia te wai mo etahi meneti. Tangohia nga arotahi whakapiri, ki te mea kei te noho me te ngawari ki te mahi. Haere tonu ki te horoi.
◆ MI TE KAUPAPA: Tangohia ki te hau hou me te okioki i te waahi pai mo te hau.
◆ Tiakina te kati.
◆ Tuhia nga ihirangi / putea kia rite ki nga tikanga o te rohe / rohe / motu / ao.

WHAKATŪPATO: Ko nga korero i whakawhiwhia ki tenei pae tukutuku i whakawhanaketia i raro i nga ritenga o te ture a te Euroopu (EU) me te tika ki to maatau mohio, korero me te whakapono i te ra i tuhia ai. Ko nga korero i homai i hangaia hei awhina mo te whakahaere me te whakamahi haumaru. Kaore e whakaarohia he waahana, he kounga kounga.

6-Iodo-3h-quinazolin-4-one(16064-08-7) Articles

Nga raupapa hou o te 4 (3H) -quinazolinone: nga whakawhitinga me te aromatawai i nga mahi antitumor me nga mahi antiviral

Ko nga raupapa hou o te 3- (3-trifluoromethylphenyl) -6-iodo-4 (3H) -quinazolinone e whai hua ana i te thiosemicarbazones, pyrazoles, he momo azomethine i te C-2 i whakahuihuihia ...

Te rangahau matū rangahau 2018 vol. 27 # 2 p. 571 - 582,

Ko te kitenga o nga tuhinga tawhito quinazolinone rite te kaha me te whiriwhiri PI3Kδ me te PI3Kδ / γ inhibitors

Ko te PI3Kδ me te PI3Kγ e whakarite ana i te taatai ​​pūtau mate. Ko te PI3Kδ, ko te PI3Kγ ranei nga kaiwhiwhi me nga kaipupuri o te PI3Kδ / γ e rua e kaha ana mo te maimoatanga o nga mate matearea-a-mate me te haumaru o te rongoā ...

Ko te Purorangi o te Tikanga Hauora 2018. 151 p. 9 - 17,

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6-Iodo-3h-quinazolin-4-one (16064-08-7) Whakahua Puku & Tauira:

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