Category: 1145671-36-8

SDS of cas: 1145671-36-8. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 4-Chloroquinazoline-6,7-diol, is researched, Molecular C8H5ClN2O2, CAS is 1145671-36-8, about Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines. Author is Asquith, Christopher R. M.; Fleck, Neil; Torrice, Chad D.; Crona, Daniel J.; Grundner, Christoph; Zuercher, William J..

We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline scaffold arrays yielded compounds with high potency and the identification of 6,7-dimethoxy-N-(4-((4-methylbenzyl)oxy)phenyl)quinolin-4-amine (34) with an MIC90 value of 0.63-1.25 μM. We also defined a series of key structural features, including the benzyloxy aniline and the 6,7-dimethoxy quinoline ring, that are important for Mtb inhibition. Importantly the compounds showed very limited toxicity and scope for further improvement by iterative medicinal chem.

In some applications, this compound(1145671-36-8)SDS of cas: 1145671-36-8 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines, published in 2019, which mentions a compound: 1145671-36-8, mainly applied to anti tubercular anilinoquinoline anilinoquinazoline, HPLC of Formula: 1145671-36-8.

We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline scaffold arrays yielded compounds with high potency and the identification of 6,7-dimethoxy-N-(4-((4-methylbenzyl)oxy)phenyl)quinolin-4-amine (34) with an MIC90 value of 1.25-2.5 μM. We also define a series of key structural features including the benzyloxy aniline and the 6,7-dimethoxy quinoline ring that are important for Mtb inhibition. Importantly the compounds showed very limited toxicity and scope for further improvement by iterative medicinal chem.

In some applications, this compound(1145671-36-8)HPLC of Formula: 1145671-36-8 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Computed Properties of C8H5ClN2O2. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 4-Chloroquinazoline-6,7-diol, is researched, Molecular C8H5ClN2O2, CAS is 1145671-36-8, about Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. Author is Tsang, Jonathan E.; Urner, Lorenz M.; Kim, Gyudong; Chow, Kingsley; Baufeld, Lynn; Faull, Kym; Cloughesy, Timothy F.; Clark, Peter M.; Jung, Michael E.; Nathanson, David A..

The epidermal growth factor receptor (EGFR) is genetically altered in nearly 60% of glioblastoma tumors; however, tyrosine kinase inhibitors (TKIs) against EGFR have failed to show efficacy for patients with these lethal brain tumors. This failure is attributed to the inability of clin. tested EGFR TKIs to cross the blood-brain barrier (BBB) and achieve adequate pharmacol. levels to inhibit various oncogenic forms of EGFR that drive glioblastoma. Through SAR anal., we developed compound 5 (JCN037)(I) from an anilinoquinazoline scaffold by ring fusion of the 6,7-dialkoxy groups to reduce the number of rotatable bonds and polar surface area and by introduction of an ortho-fluorine and meta-bromine on the aniline ring for improved potency and BBB penetration. Relative to the conventional EGFR TKIs erlotinib and lapatinib, JCN037 displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.

From this literature《Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors》,we know some information about this compound(1145671-36-8)Computed Properties of C8H5ClN2O2, but this is not all information, there are many literatures related to this compound(1145671-36-8).

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Min, Jaeki; Guo, Kexiao; Suryadevara, Praveen K.; Zhu, Fangyi; Holbrook, Gloria; Chen, Yizhe; Feau, Clementine; Young, Brandon M.; Lemoff, Andrew; Connelly, Michele C.; Kastan, Michael B.; Guy, R. Kiplin published an article about the compound: 4-Chloroquinazoline-6,7-diol( cas:1145671-36-8,SMILESS:OC1=CC2=C(Cl)N=CN=C2C=C1O ).Application of 1145671-36-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1145671-36-8) through the article.

We previously reported a novel inhibitor of the ataxia-telangiectasia mutated (ATM) kinase, which is a target for novel radiosensitizing drugs. While our initial lead, compound 4, was relatively potent and nontoxic, it exhibited poor stability to oxidative metabolism and relatively poor selectivity against other kinases. The current study focused on balancing potency and selectivity with metabolic stability through structural modification to the metabolized site on the quinazoline core. We performed extensive structure-activity and structure-property relationship studies on this quinazoline ATM kinase inhibitor in order to identify structural variants with enhanced selectivity and metabolic stability. We show that, while the C-7-methoxy group is essential for potency, replacing the C-6-methoxy group considerably improves metabolic stability without affecting potency. Promising analogs 20, 27g, and 27n were selected based on in vitro pharmacol. and evaluated in murine pharmacokinetic and tolerability studies. Compound 27g possessed significantly improve pharmacokinetics relative to that of 4. Compound 27g was also significantly more selective against other kinases than 4. Therefore, 27g is a good candidate for further development as a potential radiosensitizer.

If you want to learn more about this compound(4-Chloroquinazoline-6,7-diol)Application of 1145671-36-8, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(1145671-36-8).

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics