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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 32, 2017 - Issue 1
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Research Article

Synthesis of new pyridothienopyrimidinone derivatives as Pim-1 inhibitors

Bassem H. NaguibPharmaceutical Chemistry Department, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt; ;Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt;
,
Hala B. El-NassanPharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt; Correspondence[email protected]
&
Tamer M. AbdelghanyDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
Pages 457-467 | Received 09 Jul 2016, Accepted 08 Nov 2016, Published online: 18 Jan 2017

Figures & data

Figure 1. Pim-1 inhibitors under clinical and preclinical studies.

Figure 1. Pim-1 inhibitors under clinical and preclinical studies.

Figure 2. Designing pyridothienopyrimidinones as Pim-1 inhibitors.

Figure 2. Designing pyridothienopyrimidinones as Pim-1 inhibitors.

Figure 3. Examples of benzothienopyrimidinones and benzofuropyrimidinones as Pim-1 inhibitors.

Figure 3. Examples of benzothienopyrimidinones and benzofuropyrimidinones as Pim-1 inhibitors.

Scheme 1. Synthesis of the starting compounds 1–5.

Scheme 1. Synthesis of the starting compounds 1–5.

Scheme 2. Synthesis of the target compounds 6–8.

Scheme 2. Synthesis of the target compounds 6–8.

Scheme 3. Synthesis of the target compounds 9–11.

Scheme 3. Synthesis of the target compounds 9–11.

Figure 4. Percent inhibition of the test compounds and staurosporine (Sta) against pim-1 kinase.

Figure 4. Percent inhibition of the test compounds and staurosporine (Sta) against pim-1 kinase.

Table 1. Results of pim-1 kinase inhibition achieved by the test compounds at 50 μM.

Figure 5. IC50 in μM of compounds 6c, 7a, 7c, 7d, 8b and 9 on three cell lines.

Figure 5. IC50 in μM of compounds 6c, 7a, 7c, 7d, 8b and 9 on three cell lines.

Table 2. Results of in vitro cytotoxic screening of compounds 6c, 7a, 7c, 7d, 8b and 9 on three cell lines.

Related Research Data

In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates.
Source: MDPI AG

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